Fluoxetine blocks cloned neuronal A-type K+ channels Kvl-4

被引：21

作者：

Choi, BH ^{[1
]}

Choi, JS ^{[1
]}

Ahn, HS ^{[1
]}

Kim, MJ ^{[1
]}

Rhie, DJ ^{[1
]}

Yoon, SH ^{[1
]}

Min, DS ^{[1
]}

Jo, YH ^{[1
]}

Kim, MS ^{[1
]}

Hahn, SJ ^{[1
]}

机构：

[1] Catholic Univ Korea, Coll Med, Med Res Ctr, Dept Physiol, Seoul 137701, South Korea

来源：

NEUROREPORT | 2003年 / 14卷 / 18期

关键词：

A-type K+ current; fluoxetine; Kvl.4;

D O I：

10.1097/00001756-200312190-00032

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

The effects of fluoxetine were studied on cloned K+ channel Kvl.4 stably expressed in Chinese hamster ovary (CHO) cells using the whole-cell configuration of the patch-clamp technique. Extracellular application of various concentrations of fluoxetine inhibited the amplitude of the peak current of Kvl.4 and accelerated its inactivation time course in a concentration-dependent manner. Thus, fluoxetine decreased Kvl.4 (the integral of the outward current) in a concentration-dependent manner; the IC50 was 33.1 +/- 2.5 V M. The inhibitory effect of fluoxetine was time-dependent. The apparent association (k) and dissociation (1) rate constants measured at +40 mV were 3.5 +/- 0.7 muM(-1) s(-1) and 132.5 +/- 13.3 s(-1), respectively. The K-d (= I/k) was 379 muM, which was close to the value obtained from the concentration-response curve. The block produced by fluoxetine increased steeply between -30 and 0 W which corresponded with the voltage range for channel opening. The fluoxetine block was constant at more depolarized potentials, suggesting that the block by fluoxetine was not voltage dependent. Our data indicate that fluoxetine blocks Kvl.4 channels by preferentially binding to open state. (C) 2003 Lippincott Williams Wilkins.

引用

页码：2451 / 2455

页数：5

共 19 条

[1] Inhibition of K+ currents of outer hair cells in guinea pig cochlea by fluoxetine [J].